Copper-Catalyzed CNH<sub>2</sub>Arylation of 2-Aminobenzimidazoles and Related C-Amino-NH-azoles
作者:Desaboini Nageswar Rao、Sk. Rasheed、Karampoori Anil Kumar、Annem Siva Reddy、Parthasarathi Das
DOI:10.1002/adsc.201600035
日期:2016.6.30
nucleophilic sites that are selectively arylated at the CNH2 position are obtained, providing an exceptional tool for rapid delivery of a diverse array of medicinally important CNH(aryl) derivatives of aminoazoles without any protection/deprotection of ring NH bonds. It is first example for the selective CNH2 arylation of 5‐aminoindazole, 4‐aminopyrazole, 5‐aminopyrazole, 9H‐purine‐6‐amine, and 1H‐pyrazolo[3
Discovery of GCC5694A: A potent and selective sodium glucose co-transporter 2 inhibitor for the treatment of type 2 diabetes
作者:Young Kyu Kong、Kwang-Seop Song、Myung Eun Jung、Misuk Kang、Hyeon Jung Kim、Min Ju Kim
DOI:10.1016/j.bmcl.2021.128466
日期:2022.1
Sodium-dependentglucoseco-transporter2 (SGLT2) has emerged as a promising drug target for the treatment of type 2 diabetes, and recently, several SGLT2inhibitors have been approved for clinical use. A series of molecules with a C-aryl glucoside scaffold was designed and synthesized for biological evaluation. Among the molecules tested, a dihydrobenzofuran-containing analog, 14g (GCC5694A), exhibited